Compositions comprising an aryl pyrazole and/or a formamidine, methods and uses thereof

a technology of arylpyrazole and formamidine, which is applied in the field of compositions comprising arylpyrazole, can solve the problems of affecting health, affecting the health of animals, and causing a lot of psychological stress, and achieves the effects of improving odor dissipation, stable synergistic composition, and superior activity against parasites

Active Publication Date: 2010-05-20
MERIAL INC
View PDF75 Cites 24 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0040]In some embodiments, the invention provides compositions and methods comprising at least one 1-arylpyrazole compound in a first veterinarily acceptable carrier and at least one formamidine compound in a second veterinarily acceptable carrier, where the compounds and veterinarily acceptable carriers are stored and administered from dual-cavity containers. The methods and compositions allow for stable synergistic compositions comprising 1-arylpyrazole compounds and formamidine compounds that have superior activity against parasites. In preferred embodiments, the 1-arylpyrazole compound is fipronil and the formamidine compound is amitraz. In some embodiments, the 1-arylpyrazole compound(s) and the corresponding carrier is administered simulta

Problems solved by technology

Animals such as mammals and birds are often susceptible to parasite infestations/infections.
Fleas are a particular problem because not only do they adversely affect the health of the animal or human, but they also cause a great deal of psychological stress.
Similarly, ticks are also harmful to the physical and psychological health of the animal or human.
However, the most serious problem associated with ticks is that they are the vector of pathogenic agents in both humans and animals.
Occasionally, these toxins are fatal to the host.
Moreover, mites and lice are particularly difficult to combat since there are very few active substances which act on these parasites and they require frequent treatment.
Likewise, farm animals are also susceptible to parasite infestations.
Ticks, such as Boophilus microplus, are particularly difficult to control because they live in the pasture where farm animals graze.
One problem associated with compositions comprising formamidine compounds, including amitraz, is the lack of long-term stability under certain conditions.
Therefore, although formamidine parasiticides, including amitraz, have considerable utility for treating and preventing parasitic infestat

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Compositions comprising an aryl pyrazole and/or a formamidine, methods and uses thereof
  • Compositions comprising an aryl pyrazole and/or a formamidine, methods and uses thereof
  • Compositions comprising an aryl pyrazole and/or a formamidine, methods and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

Stability of 1-Arylpyrazole Formulations

[0627]Compound 1 (3-cyano-1-(2-chloro-6-fluoro-4-trifluoromethylphenyl)-4-dichlorofluoromethylsulfinyl-5-methyl-1H-pyrazole) was dissolved in a solvent or a combination of two or more solvents at 10% w / w. The formulations thus prepared were analyzed, using HPLC, for the content of compound 1 as the initial timepoint reading. Then all formulations were placed at 50° C., and the content of compound 1 in each of them was analyzed at the timepoints of two, four, six and, in some cases, 10 weeks. Compound 1 showed good stability in the solvents or combinations of solvents in Table 1 below. Thus formulations of Compound 1 in the solvents / carriers identified below are shown to be sufficiently stable.

TABLE 1Stability of Formulations of comprising Compound 1Stability Evaluation of Formulations(Accelerated @ 50° C.)Compound 1 (%, w / w)Form. #Carrier DescriptionInitial2 wks4 wks6 wks10 wksAN-methylpyrrolidone8.808.788.729.198.80Bbutyl acetate / octyl acetat...

example 2

Flea and Tick Efficacy of 1-Arylpyrazole Formulations in Dogs: Study A

[0628]An initial clinical study was conducted to test the efficacy of Compound 1 (3-cyano-1-(2-chloro-6-fluoro-4-trifluoromethylphenyl)-4-dichlorofluoromethylsulfinyl-5-methyl-1H-pyrazole) against ticks and fleas in various test formulations. Five test groups and an untreated control were evaluated. Each test group included six dogs. Compound was dissolved in a solvent or a combination of two or more solvents at 10% w / w. Test articles were formulated as topical spot-on solutions containing compound 1, 10% w / v in a solvent or a combination of solvents as described above. Dogs were infested with approximately 50 ticks (Rhipicephalus sanguineus) on days −1, 7, 14, 21, 28, 35 and 42. Dogs were also infested with approximately 100 fleas (Ctenocephalides felis) on days −1, 8, 15, 22, 29, 36, and 43. Treatment was applied by parting the hair and applying the formulation directly onto the skin on one spot at the midline o...

example 3

Flea and Tick Efficacy of 1-Arylpyrazole Formulations in Dogs: Study B

[0631]A separate clinical efficacy study in dogs was designed with an untreated control group and 5 test groups treated with compound 1. Each group had six dogs. Test articles were formulated as topical spot-on solutions containing compound 1, 10-20% w / v in a solvent or a combination of solvents as described above. Dogs were infested with approximately 50 ticks (Rhipicephalus sanguineus) on days −1, 7, 14, 21, 28, 35 and 42. Dogs were also infested with approximately 100 fleas (Ctenocephalides felis) on days −1, 8, 15, 22, 29, 36, and 43. Treatment was applied by parting the hair and applying the formulation directly onto the skin on one spot at the midline of the neck, between the base of the skull and the shoulder blades. The dose rate of each of the topical solutions was 0.1 ml / kg (10 mg / kg) body weight except for treatment group 4, which received 0.2 ml / kg (20 mg / kg). The efficacy of compound 1 is shown in Tab...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
Temperatureaaaaaaaaaa
Fractionaaaaaaaaaa
Timeaaaaaaaaaa
Login to view more

Abstract

This invention relates to compositions for combating parasites in animals, comprising 1-arylpyrazole compounds alone or in combination with formamidine compounds. This invention also provides for an improved methods for eradicating, controlling, and preventing parasite infestation in an animal comprising administering the compositions of the invention to the animal in need thereof.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]The present application claims the benefit of priority to U.S. Provisional Application Nos. 61 / 116,038, filed Nov. 19, 2008; 61 / 142,561, filed Jan. 5, 2009; and 61 / 167,381, filed Apr. 7, 2009; the disclosures of which are all incorporated herein by reference in their entirety.INCORPORATION BY REFERENCE[0002]Any foregoing applications, and all documents cited therein or during their prosecution (“application cited documents”) and all documents cited or referenced in the application cited documents, and all documents cited or referenced herein (“herein cited documents”), and all documents cited or referenced in herein cited documents, together with any manufacturer's instructions, descriptions, product specifications, and product sheets for any products mentioned herein or in any document incorporated by reference herein, are hereby incorporated herein by reference, and may be employed in the practice of the invention. Reference is made to ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K31/415A01P7/00A61K31/40A01N43/56A61P33/00B65D25/04A61B19/00B65D69/00
CPCA01N43/56A61K47/08A61K31/155A01N47/02A61K9/0017A61D7/00A01N43/36A61K47/14A61K31/231A61K31/4439A01N25/02A01N37/52A01N2300/00A61K2300/00A61K31/415A61P33/00A61P33/10A61P33/14A61P43/00A61K31/4152A61K31/402A61K31/56
Inventor SOLL, MARK DAVIDCRAMER, LUIZ GUSTAVOWURTZ, PATRICEPATE, JAMESSHUB, NATALYALE HIR DE FALLOIS, LOIC PATRICKTIMMONS, PHILIP REID
Owner MERIAL INC
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products